PE20141404A1 - Derivados de tieno[3,2-d]pirimidina que tienen actividad inhibidora por las quinasas de las proteinas - Google Patents
Derivados de tieno[3,2-d]pirimidina que tienen actividad inhibidora por las quinasas de las proteinasInfo
- Publication number
- PE20141404A1 PE20141404A1 PE2014001048A PE2014001048A PE20141404A1 PE 20141404 A1 PE20141404 A1 PE 20141404A1 PE 2014001048 A PE2014001048 A PE 2014001048A PE 2014001048 A PE2014001048 A PE 2014001048A PE 20141404 A1 PE20141404 A1 PE 20141404A1
- Authority
- PE
- Peru
- Prior art keywords
- amino
- alkyl
- kinases
- pyrimidine
- proteins
- Prior art date
Links
- 108091000080 Phosphotransferase Proteins 0.000 title abstract 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title abstract 2
- 102000020233 phosphotransferase Human genes 0.000 title abstract 2
- 102000004169 proteins and genes Human genes 0.000 title abstract 2
- 108090000623 proteins and genes Proteins 0.000 title abstract 2
- 230000002401 inhibitory effect Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- -1 (4-CHLOROPHENYL) AMINO Chemical class 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 208000005718 Stomach Neoplasms Diseases 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 206010017758 gastric cancer Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 201000001441 melanoma Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 201000011549 stomach cancer Diseases 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Neurology (AREA)
- Pulmonology (AREA)
- Endocrinology (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Child & Adolescent Psychology (AREA)
- Physical Education & Sports Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Communicable Diseases (AREA)
- Ophthalmology & Optometry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE TIENO[3,2-d]PIRIMIDINA DE FORMULA (I) DONDE A ES H, ALQUILO(C1-C6), CICLOALQUILO(C3-C6), ENTRE OTROS; W ES O, S, S(O), ENTRE OTROS; X E Y SON CADA UNO CH O N; Z ES H, ALQUILO(C1-C3) O NR3R4, DONDE R3 Y R4 SON CADA UNO H, ALQUILO(C1-C6), ENTRE OTROS; R1 ES H, HALOGENO, ALQUILO(C1-C3) O ALCOXI(C1-C3); R2 ES H, HALOGENO, -CF3, -NO2, ENTRE OTROS; m ES DE 0 A 5; n ES DE 0 A 2. SON COMPUESTOS PREFERIDOS: 4-AMINO-N-(1-((4-CLOROFENIL)AMINO)-6-METILISOQUINOLIN-5-IL)TIENO[3,2-d]PIRIMIDIN-7-CARBOXAMIDA; 4-AMINO-N-(6-METIL-1-((3-(TRIFLUOROMETIL)FENIL)AMINO)ISOQUINOLIN-5-IL)TIENO[3,2-d]PIRIMIDIN-7-CARBOXAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE QUINASAS DE LAS PROTEINAS SIENDO UTILES EN EL TRATAMIENTO DEL CANCER GASTRICO, MELANOMA, PSORIASIS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR20110146818 | 2011-12-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20141404A1 true PE20141404A1 (es) | 2014-10-28 |
Family
ID=48697978
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2014001048A PE20141404A1 (es) | 2011-12-30 | 2012-12-27 | Derivados de tieno[3,2-d]pirimidina que tienen actividad inhibidora por las quinasas de las proteinas |
Country Status (32)
| Country | Link |
|---|---|
| US (2) | US9156852B2 (es) |
| EP (2) | EP2797927B1 (es) |
| JP (1) | JP5797345B2 (es) |
| KR (1) | KR101490761B1 (es) |
| CN (1) | CN104039798B (es) |
| AR (1) | AR089489A1 (es) |
| AU (1) | AU2012363558C1 (es) |
| BR (2) | BR112014015720B1 (es) |
| CA (1) | CA2859668C (es) |
| CL (1) | CL2014001729A1 (es) |
| CO (1) | CO7010840A2 (es) |
| DK (1) | DK2797927T3 (es) |
| ES (2) | ES2751608T3 (es) |
| HR (1) | HRP20191840T8 (es) |
| HU (1) | HUE045957T2 (es) |
| IL (2) | IL233441B (es) |
| IN (1) | IN2014DN06101A (es) |
| LT (1) | LT2797927T (es) |
| MX (2) | MX363659B (es) |
| MY (1) | MY170988A (es) |
| PE (1) | PE20141404A1 (es) |
| PH (1) | PH12014501504B1 (es) |
| PL (1) | PL2797927T3 (es) |
| PT (1) | PT2797927T (es) |
| RS (1) | RS59420B1 (es) |
| RU (2) | RU2625799C2 (es) |
| SG (2) | SG10201701999QA (es) |
| SI (1) | SI2797927T1 (es) |
| TW (1) | TWI462927B (es) |
| UA (1) | UA109614C2 (es) |
| WO (1) | WO2013100632A1 (es) |
| ZA (1) | ZA201405583B (es) |
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| CN106795093B (zh) | 2014-10-14 | 2019-05-28 | 先正达参股股份有限公司 | 用于制备1-(3,5-二氯苯基)-2,2,2-三氟乙酮及其衍生物的方法 |
| DK3322706T3 (da) | 2015-07-16 | 2021-02-01 | Array Biopharma Inc | Substituerede pyrazolo[1,5-a]pyridin-forbindelser som ret-kinaseinhibitorer |
| EA034440B1 (ru) | 2015-10-29 | 2020-02-07 | Эффектор Терапьютикс, Инк. | СОЕДИНЕНИЯ ПИРРОЛО-, ПИРАЗОЛО-, ИМИДАЗОПИРИМИДИНА И ПИРИДИНА, КОТОРЫЕ ИНГИБИРУЮТ Mnk1 И Mnk2 |
| EP3368530A1 (en) | 2015-10-29 | 2018-09-05 | Effector Therapeutics Inc. | Isoindoline, azaisoindoline, dihydroindenone and dihydroazaindenone inhibitors of mnk1 and mnk2 |
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| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| US11440898B2 (en) * | 2016-12-28 | 2022-09-13 | Minoryx Therapeutics S.L. | Isoquinoline compounds, methods for their preparation, and therapeutic uses thereof in conditions associated with the alteration of the activity of beta galactosidase |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
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| TWI762579B (zh) | 2017-02-14 | 2022-05-01 | 美商伊凡克特治療公司 | 六氫吡啶經取代之ＭｎＫ抑制劑及其相關方法 |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| MY198379A (en) | 2017-07-28 | 2023-08-28 | Yuhan Corp | Improved Process for Preparing Aminopyrimidine Derivatives |
| TW202428305A (zh) | 2017-09-08 | 2024-07-16 | 美商建南德克公司 | 癌症之診斷及治療方法 |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
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| CA3087354C (en) | 2018-01-18 | 2023-01-03 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
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| US20210008047A1 (en) | 2018-02-13 | 2021-01-14 | Vib Vzw | Targeting minimal residual disease in cancer with rxr antagonists |
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| CN114213430B (zh) * | 2021-12-28 | 2022-12-02 | 深圳湾实验室 | 4-氨基噻吩[3,2-d]嘧啶-7-羧酸的制备方法、蛋白激酶抑制剂中间体 |
| CN114524826A (zh) * | 2022-02-18 | 2022-05-24 | 郑州猫眼农业科技有限公司 | 7-溴-4-氯噻吩并[3,2-d]嘧啶的制备工艺 |
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| GB0402518D0 (en) * | 2004-02-05 | 2004-03-10 | Astrazeneca Ab | Therapeutic agents |
| GB0512324D0 (en) | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
| RU2528046C2 (ru) * | 2004-06-24 | 2014-09-10 | Вертекс Фармасьютикалз Инкорпорейтед | Модуляторы транспортеров атф-связывающей кассеты |
| MY146795A (en) | 2005-06-09 | 2012-09-28 | Novartis Ag | Process for the synthesis of organic compounds |
| US7989461B2 (en) | 2005-12-23 | 2011-08-02 | Amgen Inc. | Substituted quinazolinamine compounds for the treatment of cancer |
| RU2008140382A (ru) * | 2006-03-16 | 2010-04-27 | Новартис АГ (CH) | Гетероциклические органические соединения, например, для лечения меланомы |
| EA200802118A1 (ru) * | 2006-04-07 | 2009-04-28 | Девелоджен Ациенгезельшафт | Обладающие ингибирующей активностью в отношении mnk1/mnk2 тиенопиримидины, предназначенные для применения в фармацевтических композициях |
| WO2008044688A1 (en) * | 2006-10-11 | 2008-04-17 | Daiichi Sankyo Company, Limited | Urea derivative |
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| KR20110100241A (ko) * | 2008-12-05 | 2011-09-09 | 아르퀼 인코포레이티드 | Ｒａｆ 억제제 및 이들의 용도 |
| JP5645839B2 (ja) | 2009-03-05 | 2014-12-24 | 武田薬品工業株式会社 | Ｃｄｃ７キナーゼ阻害剤としてのチエノピリミジン |
| DE102009035754A1 (de) | 2009-07-24 | 2011-01-27 | Hartmetall-Werkzeugfabrik Paul Horn Gmbh | Schneideinsatz für ein Schneidwerkzeug zur spanenden Bearbeitung, insbesondere zum Hochvorschubfräsen |
| JP2013503188A (ja) * | 2009-08-28 | 2013-01-31 | アレイ バイオファーマ、インコーポレイテッド | Ｒａｆ阻害化合物およびその使用方法 |
| KR101147550B1 (ko) * | 2009-10-22 | 2012-05-17 | 한국과학기술연구원 | 단백질 키나아제 저해활성을 가지는 2,7-치환된 티에노［3,2-ｄ］피리미딘 화합물 |
| KR101094446B1 (ko) * | 2009-11-19 | 2011-12-15 | 한국과학기술연구원 | 단백질 키나아제 저해활성을 가지는 2,4,7-치환된 티에노［3,2-ｄ］피리미딘 화합물 |
| EP2528925B1 (en) | 2010-01-29 | 2017-07-05 | Hanmi Science Co., Ltd. | THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY ON PROTEIN KINASES |
| KR101483215B1 (ko) | 2010-01-29 | 2015-01-16 | 한미약품 주식회사 | 단백질 키나아제 저해활성을 갖는 비시클릭 헤테로아릴 유도체 |
| KR101995013B1 (ko) * | 2010-07-13 | 2019-07-02 | 에프. 호프만-라 로슈 아게 | Irak4 조절제로서 피라졸로[1,5a]피리미딘 및 티에노[3,2b]피리미딘 유도체 |
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